Tag: Anticancer

Lexatumumab (HGS 1018) is a TRAIL-R2 Agonist Antibody

TRAIL-R2 (TNF-related apoptosis-inducing ligand receptor 2), also known as death receptor 5 (DR5), is a cell surface receptor that binds TRAIL, a cytokine that causes apoptosis. Additionally, TRAIL-R2 contains two extracellular cysteine-rich repeats and a cytoplasmic death domain. The receptor engages a caspase-dependent apoptotic pathway. It mediates apoptosis via...

Bapotulimab (BAY-1905254) is an IgG2 Antibody Targeting ILDR2

Immunoglobulin-like domain containing receptor 2 (ILDR2) is a B7-like protein that belongs to the B7 family of immunomodulatory receptors. It can induce an immunosuppressive effect on T-cell responses. ILDR2 is a negative regulator for T cells. Besides, ILDR2 is expressed in immune cells and in immune-privileged and inflamed tissues....

Tigatuzumab (CS-1008) is a Humanized Death Receptor 5 (DR5) IgG1 mAb

Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL), a member of the TNF superfamily of cytokines, is a type 2 membrane protein expressed in the majority of normal tissues. TRAIL can undergo protease cleavage, resulting in a soluble form able to bind to TRAIL death receptors (DRs). Moreover, TRAIL induces apoptosis...

NecroIr2 is an Iridium(III) Complex, Can be Used as an Anticancer Agent

Inorganic elements play crucial roles in biomedical processes. Many inorganic elements such as transition metals have anticancer activities. Even though metal complexes are making progress against cancer, cisplatin (CDDP) remains the most widely used first-line chemotherapeutic drug for various cancers. Drug resistance to cisplatin significantly limits its clinical use...

A947 is a Selective and Efficacious SMARCA2 PROTAC in SMARCA4 Mutant Cancers

SWI/SNF complex has two important ATP-dependent helicases, SMARCA2 and SMARCA4. In fact, SMARCA2 and SMARCA4 share strong protein sequence homology.  But SWI/SNF helicase SMARCA4 is frequently mutated in cancer. The inactivation of SMARCA4 results in a cellular dependence on SMARCA2. Thus, SMARCA2 becomes an attractive synthetic lethal target. Proteolysis...

Mogamulizumab is a Defucosylated Anti-CCR4 Monoclonal Antibody

C-C Motif Chemokine Receptor 4 (CCR4) is a G-coupled-protein receptor for C-C chemokines. It’s on surface of tumor cells in leukemia and lymphoma patients. For example, adult T-cell leukemia-lymphoma (ATLL), peripheral T-cell lymphoma (PTCL) and cutaneous T-cell lymphoma (CTCL) all expresses CCR-4. Furthermore, leukemia and lymphoma are clinically and...

Targefrin is a Potent EphA2 Antagonist with Antitumor Activity

EphA2, a transmembrane glycoprotein, is a type of Ephrin receptors (Eph) which is the most important class of receptor tyrosine kinases. EphA2 can be detected in most epithelial cells. In common situation, it interacts with ephrin A1 on the neighboring cell, thereby inducing diverse signaling networks following cell-to-cell contact. Ephrin...